WO2014149140A2 - Système d'administration comprenant de l'acide ascorbique stabilisé et d'autres principes actifs - Google Patents

Système d'administration comprenant de l'acide ascorbique stabilisé et d'autres principes actifs Download PDF

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Publication number
WO2014149140A2
WO2014149140A2 PCT/US2014/000062 US2014000062W WO2014149140A2 WO 2014149140 A2 WO2014149140 A2 WO 2014149140A2 US 2014000062 W US2014000062 W US 2014000062W WO 2014149140 A2 WO2014149140 A2 WO 2014149140A2
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WO
WIPO (PCT)
Prior art keywords
formulation
group
dispersant
mixtures
combination
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
Application number
PCT/US2014/000062
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English (en)
Other versions
WO2014149140A3 (fr
Inventor
Julius Zecchino
Alexander ZECCHINO
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Individual
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Individual
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Individual filed Critical Individual
Publication of WO2014149140A2 publication Critical patent/WO2014149140A2/fr
Publication of WO2014149140A3 publication Critical patent/WO2014149140A3/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/72Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
    • A61K8/84Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds obtained by reactions otherwise than those involving only carbon-carbon unsaturated bonds
    • A61K8/89Polysiloxanes
    • A61K8/891Polysiloxanes saturated, e.g. dimethicone, phenyl trimethicone, C24-C28 methicone or stearyl dimethicone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/58Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing atoms other than carbon, hydrogen, halogen, oxygen, nitrogen, sulfur or phosphorus
    • A61K8/585Organosilicon compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/67Vitamins
    • A61K8/676Ascorbic acid, i.e. vitamin C
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q17/00Barrier preparations; Preparations brought into direct contact with the skin for affording protection against external influences, e.g. sunlight, X-rays or other harmful rays, corrosive materials, bacteria or insect stings
    • A61Q17/04Topical preparations for affording protection against sunlight or other radiation; Topical sun tanning preparations

Definitions

  • the present invention relates a delivery system with actives such as ascorbic acid that retain their stability, functionality and aesthetics.
  • a formulation and related method of manufacture comprising: at least one elastomer; a first dispersant; a second dispersant and at least one active wherein the formulation forms a delivery system wherein the active in the formulation retains its stability, functionality and aesthetics.
  • the present invention provides for a delivery system wherein the water soluble antioxidant retains its stability ! functionality and aesthetics.
  • the present invention provides for a formulation comprising: at least one elastomer; a first dispersant; a second dispersant and at least one active wherein the formulation forms a delivery system wherein the active in the formulation retains its stability, functionality and aesthetics.
  • the elastomer is selected from a group consisting essentially of Dimethicone, Dimethicone Copolymers, Vinyldimethicone Copolymers and cross polymers, Silicone, and combination and mixtures thereof.
  • the term "elastomer” is defined as any natural or synthetic material, including polymers, that is able to resume its original shape when a deforming force is removed.
  • the first dispersant is selected from a group consisting essentially of Cyclomethicone, Isododecane, Hydrocarbons, Esters, Dimethicones, petrolatum, Cyclopentasiloxane, and combination and mixtures thereof.
  • the second dispersant is selected from a group consisting essentially of Dimethicone, Cyclomethicones, Hydrocarbons, Esters, and combination and mixtures thereof.
  • the term "dispersant” is defined as a liquid or gas added to a mixture to promote dispersion or maintain dispersed particles in suspension and also includes any material that is able to gel the elastomer dispersed in it while keeping its structure and stability over time.
  • the active is selected from a group consisting essentially of Ascorbic Acid, Epigallo Catechin Gallate (EGCG), Hydroquinone, Ubiquinone, Ubiquinol, Ferrulic Acid, Lipoic acid, and combination and mixtures thereof.
  • EGCG Epigallo Catechin Gallate
  • Hydroquinone Hydroquinone
  • Ubiquinone Ubiquinol
  • Ferrulic Acid Lipoic acid
  • the formulation can be used as a product selected from a group consisting of skin care products, cosmetics, cosmeceuticals, pharmaceuticals and nutriceuticats.
  • the formulation can be combined with other components and ingredients to form a product selected from a group consisting of skin care products, cosmetics, cosmeceuticals, pharmaceuticals and nutriceuticals.
  • the formulation further comprises an activator selected from a group consisting essentially of Water, Glycerin, Glycols, Polyols, Polyglutamic Acid, Hyaluronic Acid, and combination and mixtures thereof.
  • the formulation further comprises at least one anhydrous system such as bentone cyclomethicone gel with organic sunscreens.
  • anhydrous is defined as any non-aqueous (no water) or limited water containing formulation or composition.
  • the second dispersant has a viscosity from about 0.65 to about 350 centistoke.
  • the present invention provides for a formulation manufactured by a process comprising; admixing at least one elastomer with a first dispersant to form a gel; admixing a second dispersant with the gel; and admixing at least one active with the gel to form a delivery system with an active in the formulation retains its stability, functionality and aesthetics.
  • the second dispersant has a viscosity from about 0.65 to about 20 centistoke.
  • the process further comprises admixing at least one sunscreen formulation.
  • the present invention relates to a formulation containing ascorbic acid, and the formulation comprises: at least one elastomer; a first dispersant; a silicone and ascorbic acid wherein the formulation forms a delivery system wherein the ascorbic acid in the formulation retains its stability, functionality and aesthetics.
  • the present invention provides for a formulation manufactured by a process comprising: admixing at least one elastomer with a first dispersant to form a gel; admixing a silicone with the gel; and admixing ascorbic acid with the gel to form a delivery system with an active in the formulation retains its stability, functionality and aesthetics.
  • the process further comprises admixing at least one activator selected from a group consisting essentially of Water, Glycerin, Glycols, Polyols, Polyglutamic Acid, Hyaluronic Acid, and combination and mixtures thereof.
  • the focus of the present invention is stabilizing, inherently, unstable water-soluble anti-oxidants or actives such as Ascorbic Acid (AA), Epigallocatcchin Gallate (EGCG), and N-acctyl glucosamine (NAG).
  • actives help to protect the skin when applied topically, by reducing the action of free radicals that can cause harm to cells.
  • AA Ascorbic Acid
  • EGCG Epigallocatcchin Gallate
  • NAG N-acctyl glucosamine
  • the present invention provides for a solution using gels.
  • the selection of the gelling agent is critical. If the vehicle is too thin, the materials will sink to the bottom and the formula will not be homogeneous, and will not be able to deliver proper doses to the skin. If the vehicle is too thick, it will not apply evenly and the consumer/end user will not like the "feel .
  • a gel having a cream-like consistency is optimal. It allows the consumer to apply and enjoy the comfort and benefit of the therapy.
  • the presently claimed invention uses Elastomer technology to achieve the desired results. Dimethicon/vinyldimethicone crosspolymers have been used in cosmetics to create great texture and feel. Interestingly, when one of these molecules is added to the different elastomer gels, the combination is stable but is aesthetically undesirable because you can feel the scratchincss of the dispersed materials. Therefore the right dispersing agents must be used to not only gel the elastomer, but to enable the active materials to blend into the base homogeneously.
  • the present invention has shown that using Isododecane and Cyclopetasiloxane, and Dimettcone 5cps provides for desired results.
  • a second dispersant is used to fine tune the right consistency.
  • Elastomers are silicone rubbers that have been used in many industries.
  • the finished formula we have is cosmetically commercial and viable. It efficiently stabilizes the actives until they reach the skin.
  • the water proof film that is left on the skin after it is applied not only is silky smooth and desirable but helps to aid the penetration and keep the active in place, until it can be absorbed.
  • Phase A is weighed in kettle equipped with a high speed agitation. Phase B is then added to Phase A and mixed until homogeneous. Phase C is then slowly admixed with Phase AB and then mixed on very high speed.
  • the ingredients and % of each ingredient in the composition is set forth below in Table 1.
  • Phase A is weighed in kettle equipped with a high speed agitation. Phase B is then added to Phase A and mixed until homogeneous. Phase C is then slowly admixed with Phase AB and then mixed on very high speed.
  • the ingredients and 1 ⁇ 2 of each ingredient in the composition is set forth below in Table 2.
  • Phase ⁇ is weighed in kettle equipped with a high speed agitation. Phase B is then added to Phase A and mixed until homogeneous. Phase C is then slowly admixed with Phase AB and then mixed on very high speed.
  • the ingredients and % of each ingredient in the composition is set forth below in Table 3.
  • Phase A is weighed in kettle equipped with a high speed agitation. Phase B is then added to Phase A and mixed until homogeneous. Phase C is then slowly admixed with Phase AB and then mixed on very high speed.
  • the ingredients and % of each ingredient in the composition is set forth below in Table 4.
  • Stability tests were also conducted over a six month period and the tests results showed no deterioration of the actives.
  • the stability tests are set for the below in Table 5: ICC STABILIZED ACTIVE STABILITY DATA

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Birds (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Cosmetics (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

La présente invention concerne une préparation fabriquée selon un procédé consistant à : mélanger au moins un élastomère avec un premier agent dispersant pour former un gel ; mélanger un second agent dispersant avec le gel ; et mélanger au moins un principe actif, tel que l'acide ascorbique, avec le gel pour former un système d'administration où le principe actif présent dans la préparation conserve sa stabilité, sa fonctionnalité et son aspect.
PCT/US2014/000062 2013-03-21 2014-03-21 Système d'administration comprenant de l'acide ascorbique stabilisé et d'autres principes actifs Ceased WO2014149140A2 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US13/816,000 2013-03-21
US13/816,000 US9132080B2 (en) 2013-03-21 2013-03-21 Delivery system having stabilized ascorbic acid and other actives

Publications (2)

Publication Number Publication Date
WO2014149140A2 true WO2014149140A2 (fr) 2014-09-25
WO2014149140A3 WO2014149140A3 (fr) 2014-11-27

Family

ID=51569285

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2014/000062 Ceased WO2014149140A2 (fr) 2013-03-21 2014-03-21 Système d'administration comprenant de l'acide ascorbique stabilisé et d'autres principes actifs

Country Status (2)

Country Link
US (1) US9132080B2 (fr)
WO (1) WO2014149140A2 (fr)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9144564B2 (en) * 2013-03-21 2015-09-29 Julius Zecchino Delivery system having stabilized ascorbic acid and other actives
WO2021212073A1 (fr) 2020-04-16 2021-10-21 Baek Clinical Inc. Formulations topiques à haute puissance de vitamine c et d'alcool-sucre
AU2021255734A1 (en) 2020-04-16 2022-11-24 Mf Beauty Partners Llc Stabilizing vitamin C application formulations

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0545002A1 (fr) * 1991-11-21 1993-06-09 Kose Corporation Polymère de silicone, composition pâteuse et composition cosmétique du type eau-dans-l'huile le contenant
ZA971943B (en) * 1996-06-28 1998-09-07 Unilever Plc Vitamin C delivery system
WO1999013859A1 (fr) * 1997-09-16 1999-03-25 E-L Management Corp. Formulation anhydre stable
FR2791566B1 (fr) * 1999-03-31 2001-05-11 Oreal Composition contenant un actif instable en milieu oxydant, et ses utilisations notamment cosmetiques
US6267974B1 (en) * 1999-04-16 2001-07-31 Unilever Home & Personal Care Usa, Division Of Conopco, Inc. Cosmetic compositions with sensate mixtures based on isopulegol
US6649178B2 (en) * 2000-06-13 2003-11-18 Fatemeh Mohammadi Cosmetic composition for stressed skin under extreme conditions
US6524598B2 (en) * 2000-07-10 2003-02-25 The Procter & Gamble Company Cosmetic compositions
JP4276179B2 (ja) * 2002-11-04 2009-06-10 ザ プロクター アンド ギャンブル カンパニー 改善された安定性を有し、クレンジング相と別個の効能相(abenefitphase)とを含有する、ストライプ模様の液体パーソナルクレンジング組成物
EP2168633B1 (fr) * 2008-09-30 2016-03-30 L'Oréal Composition cosmétique comprenant un composé organique du silicium comportant au moins une fonction basique, un polymère filmogène hydrophobe, un pigment et un solvant volatil

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Publication number Publication date
US9132080B2 (en) 2015-09-15
WO2014149140A3 (fr) 2014-11-27
US20140286882A1 (en) 2014-09-25

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